2-[[6-methyl-5-[2-[(Z)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic acid | 176391-41-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-[[6-methyl-5-[2-[(Z)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic acid
• 英文别名: 2-[[6-methyl-5-[2-[(E)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic acid
• CAS: 176391-41-6
• 化学式: C₂₇H₂₆N₂O₄
• 分子量: 442.5
• InChiKey: VSVQEQDGOFPGAT-ORIPQNMZSA-N

物化性质

• 熔点：
  147-158 °C(lit.)
• 沸点：
  635.7±65.0 °C(Predicted)
• 密度：
  1.21±0.1 g/cm3(Predicted)
• 溶解度：
  二甲基亚砜：18 毫克/毫升

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  33
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  81
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• SUSTAINED RELEASE PREPARATION FOR TISSUE REGENERATION THERAPY
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2087890A1

  公开（公告）日：2009-08-12

  The object of the present invention is to provide a microsphere which has a slow-release period of from about two weeks to about four weeks following administration, enables a higher content of a drug to be included, suppresses an initial burst of the drug, and enables the drug to be maintained at an optimal, effective blood concentration during the slow-release period. In a microsphere containing a drug and PLGA, the above problems can be resolved by setting: (1) the amount of lactic acid/glycolic acid copolymer per part by weight of the drug to from about 3 to about 10 parts by weight; (2) the microsphere to an average particle size of from about 20 to about 50 µm; and (3) the lactic acid/glycolic acid copolymer to a weight-average molecular weight of from about 10,000 to about 50,000 and to a lactic acid/glycolic acid compositional ratio of from about 75/25 to about 50/50. In addition, the microsphere, by promoting the production of various endogenous repair factors, is useful against various tissue disorders.

  本发明的目的是提供一种微球，该微球在给药后具有约两周到四周的缓释期，能够包含较高含量的药物，抑制药物的初始迸发，并使药物在缓释期保持在最佳的有效血药浓度。 在含有药物和 PLGA 的微球中，可以通过设置以下条件来解决上述问题：(1) 每份药物重量的乳酸/乙醇酸共聚物的量为约 3 至约 10 份重量；(2) 微球的平均粒径为约 20 至约 50 微米；(3) 乳酸/乙醇酸共聚物的重量平均分子量为约 10,000 至约 50,000 和乳酸/乙醇酸的组成比例为约 75/25 至约 50/50。 此外，微球通过促进各种内源性修复因子的产生，可用于防治各种组织疾病。
• MEDICINAL COMPOSITION FOR TREATING INTRACTABLE HEART DISEASE
  申请人：Osaka University

  公开号：EP3569249A1

  公开（公告）日：2019-11-20

  The present invention provides a pharmaceutical composition for use in treating an intractable heart tissue fibrosis disease accompanied by chronic heart failure. The pharmaceutical composition for use in treating an intractable heart tissue fibrosis disease accompanied by chronic heart failure comprises, as an active ingredient, at least one member selected from the group consisting of protease inhibitors, thromboxane A2 synthase inhibitors, thromboxane A2 synthase antagonists, phosphodiesterase (PDE) inhibitors, tyrosine kinase inhibitors, HMG-CoA reductase inhibitors, and antifibrotic agents. (The pharmaceutical composition includes biodegradable polymer-encapsulated, long-acting preparations thereof.)

  本发明提供了一种用于治疗伴有慢性心力衰竭的难治性心脏组织纤维化疾病的药物组合物。用于治疗伴有慢性心力衰竭的难治性心脏组织纤维化疾病的药物组合物包括至少一种选自由蛋白酶抑制剂、血栓素 A2 合酶抑制剂、血栓素 A2 合酶拮抗剂、磷酸二酯酶 (PDE) 抑制剂、酪氨酸激酶抑制剂、HMG-CoA 还原酶抑制剂和抗纤维化剂组成的组的成员作为活性成分。(药物组合物包括其中的生物可降解聚合物包封长效制剂）。
• DISEASE-SITE-SPECIFIC LIPOSOMAL FORMULATION
  申请人：Osaka University

  公开号：EP3718537A1

  公开（公告）日：2020-10-07

  The present invention provides a clinically applicable, safe and convenient, pharmaceutical composition for disease site-specific treatment. The pharmaceutical composition for disease site-specific treatment comprises a stealth liposome having a prostaglandin I2 receptor agonist encapsulated therein.

  本发明提供了一种临床适用、安全方便、用于疾病部位特异性治疗的药物组合物。这种用于疾病部位特异性治疗的药物组合物包括一种隐形脂质体，其中封装有前列腺素 I2 受体激动剂。
• Sustained release preparation for tissue regeneration therapy
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2087890B1

  公开（公告）日：2014-03-05
• Medicinal Composition for Treating Intractable Heart Disease
  申请人：Osaka University

  公开号：US20190343841A1

  公开（公告）日：2019-11-14

  The present invention provides a pharmaceutical composition for use in treating an intractable heart tissue fibrosis disease accompanied by chronic heart failure. The pharmaceutical composition for use in treating an intractable heart tissue fibrosis disease accompanied by chronic heart failure comprises, as an active ingredient, at least one member selected from the group consisting of protease inhibitors, thromboxane A 2 synthase inhibitors, thromboxane A 2 synthase antagonists, phosphodiesterase (PDE) inhibitors, tyrosine kinase inhibitors, HMG-CoA reductase inhibitors, and antifibrotic agents. (The pharmaceutical composition includes biodegradable polymer-encapsulated, long-acting preparations thereof.)